Oral W/O microemulsion preparation of cyclo-trans-4-hydroxyprolyl-L-serine and preparation method of same

Abstract

The invention discloses an oral W / O microemulsion preparation of cyclo-trans-4-hydroxyprolyl-L-serine, which is advantageous in that the half-life period of cyclo-trans-4-hydroxyprolyl-L-serine is prolonged and the oral bioavailability of cyclo-trans-4-hydroxyprolyl-L-serine is improved. The oral W / O microemulsion preparation contains the following components in percentage by weight: 0.3% to 0.4% of cyclo-trans-4-hydroxyprolyl-L-serine, 10% to 40% of medicinal oil, 10% to 50% of emulsifiers, 10% to 50% of anhydrous ethanol and deionized water. The preparation method comprises the following steps: thoroughly mixing emulsifiers, anhydrous ethanol and medicinal oil at the given ratio to obtain an oil phase; adding the given amount of cyclo-trans-4-hydroxyprolyl-L-serine into deionized water and dissolving thoroughly to obtain a water phase; and slowly adding the water phase into the oil phase while magnetically stirring, and stopping stirring until a clear oily liquid is obtained.

Description

technical field [0001] The invention relates to a hyseride preparation, in particular to an oral hyseride W / O microemulsion preparation capable of prolonging the half-life of the hyseride and improving the oral bioavailability of the hyseride and a preparation method thereof. Background technique: [0002] Hydroxyserin, whose chemical name is cyclotrans-4 L-hydroxyprolylserine, is an active dipeptide extracted and isolated from the Japanese anti-hepatitis drug Laennec (trade name of human placental hydrolyzate). Its chemical structure is as follows : [0003] [0004] At present, Hydroxyserin is artificially synthesized by Japan Biopharmaceuticals Co., Ltd. and has been sold publicly. Existing experiments have shown that hydroxyl serin has good anti-hepatitis activity and little adverse reaction. However, Hydroxyserin has good water solubility and small molecular weight (about 200 Daltons), which is a drug with low permeability, and the permeability coefficient is about...

AI Technical Summary

Problems solved by technology

However, Hydroxyserin has good water solubility and small molecular weight (about 200 Daltons), which is a drug with low permeability, and the permeability coefficient is about 5.01×10 -6 (cm / sec), that is, the membrane permeability of oral drugs is poor, and it is difficult to pass through the biofilm barrier

In addition, due to the presence of a large number of peptidases and proteolytic enzymes in the gastrointestinal tract, direct oral administration of hydroxyl silk peptide is prone to first-pass effect and is eliminated by liver metabolism.

The result of the experiment was that after the rats were directly orally administered with hydroxylase peptide, t 1 / 2 Only 30~40min, the oral absorption is incomplete, and the bioavailability is about 30%. The therapeutic effect can only be achieved through frequent administration, which is time-consuming and laborious.

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